JP2005514410A - ４−デジメチルアミノテトラサイクリン化合物 - Google Patents

４−デジメチルアミノテトラサイクリン化合物 Download PDF

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JP2005514410A
JP2005514410A JP2003557528A JP2003557528A JP2005514410A JP 2005514410 A JP2005514410 A JP 2005514410A JP 2003557528 A JP2003557528 A JP 2003557528A JP 2003557528 A JP2003557528 A JP 2003557528A JP 2005514410 A JP2005514410 A JP 2005514410A
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tetracycline compound
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aryl
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JP2005514410A5 (fr
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マーク エル． ネルソン
クワシ オーエメン
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パラテック ファーマシューティカルズ インコーポレイテッド
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/24—Esteramides
    • C07F9/2454—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/2475—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic of aralkylamines
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
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    • C07C2601/00—Systems containing only non-condensed rings
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    • C07—ORGANIC CHEMISTRY
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    • C07C2601/00—Systems containing only non-condensed rings
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    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
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    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005520846A (ja) * 2002-03-21 2005-07-14 パラテック ファーマシューティカルズ インコーポレイテッド 置換されたテトラサイクリン化合物。
JP2005526754A (ja) * 2002-03-08 2005-09-08 パラテック ファーマシューティカルズ インコーポレイテッド アミノメチル置換されたテトラサイクリン化合物
JP2010513527A (ja) * 2006-12-21 2010-04-30 パラテック ファーマシューティカルズ インコーポレイテッド 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6756365B2 (en) * 1991-11-06 2004-06-29 Trustees Of Tufts College Reducing tetracycline resistance in living cells
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
DK1240133T3 (da) * 1999-09-14 2006-08-21 Tufts College Fremgangsmåde til fremstilling af substituerede tetracycliner med overgangsmetalbaserede kemiske metoder
AU3105801A (en) * 2000-01-24 2001-07-31 Trustees Of Tufts College Tetracycline compounds for treatment of cryptosporidium parvum related disorders
KR20030007489A (ko) * 2000-03-31 2003-01-23 트러스티즈 오브 터프츠 칼리지 7- 및 9-카르바메이트, 우레아, 티오우레아,티오카르바메이트 및 헤테로아릴-아미노 치환된테트라사이클린 화합물
DE60102815D1 (de) * 2000-05-15 2004-05-19 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
US20040224927A1 (en) * 2000-06-16 2004-11-11 Trustees Of Tufts College 7-N-substituted phenyl tetracycline compounds
US20020132798A1 (en) * 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
AU2001268475A1 (en) * 2000-06-16 2002-01-02 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
SI1301467T1 (sl) 2000-07-07 2007-02-28 Tufts College 9-substituirane minociklinske spojine
US7094806B2 (en) * 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
BR0112265A (pt) * 2000-07-07 2003-06-24 Tufts College Compostos de tetraciclina substituìda, e de sanciclina 7-substituìda, método para tratar um estado responsivo à tetraciclina em um indivìduo, e, composição farmacêutica
US7553828B2 (en) 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
WO2002072506A2 (fr) * 2001-03-13 2002-09-19 Paratek Pharmaceuticals, Inc. Composes de 7-pyrollyl tetracycline et procedes d'utilisation associes
MXPA03008165A (es) 2001-03-13 2003-12-12 Paratek Pharm Innc Compuestos tetraciclina sustituidos en la posicion 7,9.
US7045507B2 (en) 2001-03-14 2006-05-16 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
US8088820B2 (en) * 2001-04-24 2012-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
US20060194773A1 (en) * 2001-07-13 2006-08-31 Paratek Pharmaceuticals, Inc. Tetracyline compounds having target therapeutic activities
EP1408987B1 (fr) * 2001-07-13 2013-04-10 Paratek Pharmaceuticals, Inc. Composes de tetracycline a activites therapeutiques cibles
WO2003055441A2 (fr) 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
AU2003235759A1 (en) * 2002-01-08 2003-07-24 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
CN1700922A (zh) * 2002-07-12 2005-11-23 帕拉特克药品公司 3、10或12a位取代的四环素化合物
CA2503446C (fr) 2002-10-24 2012-12-18 Paratek Pharmaceuticals, Inc. Procedes d'utilisation de composes tetracycline substituee pour moduler l'arn
WO2005009943A2 (fr) * 2003-07-09 2005-02-03 Paratek Pharmaceuticals, Inc. Composes de tetracycline substitues
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
EP2332904A3 (fr) 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derives des composes de tetracycline
AU2012202559B2 (en) * 2004-05-21 2014-07-17 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
AU2014250722B2 (en) * 2004-05-21 2016-05-26 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
LT1753713T (lt) 2004-05-21 2016-11-25 President And Fellows Of Harvard College Tetraciklinų ir jų analogų sintezė
TWI261038B (en) * 2004-08-11 2006-09-01 Bo-Cheng Chen Bicycle gear-shifting handgrip
EP2284164A3 (fr) 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Composés de tétracycline substituée
US7858601B2 (en) * 2004-10-25 2010-12-28 Paratek Pharmaceuticals, Inc. 4-substituted tetracyclines and methods of use thereof
JP2008530023A (ja) 2005-02-04 2008-08-07 パラテック ファーマシューティカルズ インコーポレイテッド テトラサイクリン化合物の１１ａ，１２−誘導体
AR057032A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos de preparacion
AR057033A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos para preparar 9-nitrominociclina
US20070093455A1 (en) * 2005-07-21 2007-04-26 Paul Abato 10-substituted tetracyclines and methods of use thereof
RU2008121238A (ru) * 2005-12-22 2010-01-27 Вайет (Us) Способы лечения инфекций желудочно-кишечного тракта с применением тайгециклина
BRPI0620646A2 (pt) * 2005-12-22 2011-11-22 Wyeth Corp composição farmacêutica compreendendo tigeciclina e seu uso
WO2007087416A2 (fr) * 2006-01-24 2007-08-02 Paratek Pharaceuticals, Inc. Procede permettant d'accroitre la biodisponibilite orale de tetracyclines
WO2007117639A2 (fr) 2006-04-07 2007-10-18 The President And Fellows Of Harvard College Synthèse de tétracyclines et d'analogues de celles-ci
CA2652347A1 (fr) * 2006-05-15 2007-11-22 Paratek Pharmaceuticals, Inc. Methodes de regulation de l'expression de genes ou de produits geniques a l'aide de composes de tetracycline substituee
WO2008045507A2 (fr) 2006-10-11 2008-04-17 Paratek Pharmaceuticals, Inc. Composés de tétracycline substitués utilisés pour le traitement d'infections à bacillus anthracis
EP2076133B1 (fr) 2006-10-11 2012-12-12 President and Fellows of Harvard College Synthèse d'un intermédiaire d'énone
CA2892739A1 (fr) 2006-12-21 2008-07-03 Paratek Pharmaceuticals, Inc. Utilisation de composes a base de tetracycline substituee dans le traitement d'affections cutanees inflammatoires
US7935687B2 (en) * 2007-04-12 2011-05-03 Paratek Pharmaceuticals, Inc. Methods for treating spinal muscular atrophy using tetracycline compounds
CA2706475C (fr) 2007-11-29 2016-05-03 Actelion Pharmaceuticals Ltd Derives d'acide phosphonique et leur utilisation en tant qu'antagonistes du recepteur p2y12
WO2009111064A2 (fr) 2008-03-05 2009-09-11 Paratek Pharmaceuticals, Inc. Composés de minocycline et procédés d’utilisation de ceux-ci
AU2009236631A1 (en) * 2008-04-14 2009-10-22 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
WO2010006292A1 (fr) 2008-07-11 2010-01-14 Neumedics Dérivés de tétracycline présentant une activité antibiotique réduite et des bénéfices neuroprotecteurs
JP2012503017A (ja) * 2008-09-19 2012-02-02 パラテック ファーマシューティカルズ インコーポレイテッド 関節リウマチの治療用のテトラサイクリン化合物および関連する治療方法
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto
PL2427425T3 (pl) 2009-05-08 2017-08-31 Tetraphase Pharmaceuticals, Inc. Związki tetracyklinowe
NZ740051A (en) 2012-08-31 2019-09-27 Tetraphase Pharmaceuticals Inc Tetracycline compounds
EP3529236B1 (fr) 2016-10-19 2024-02-07 Tetraphase Pharmaceuticals, Inc. Formes cristallines de l'éravacycline
SG10201913599RA (en) 2016-11-01 2020-02-27 Paratek Pharm Innc 9-aminomethyl minocycline compounds and use thereof in treating community-acquired bacterial pneumonia (cabp)
AU2021233829A1 (en) * 2020-03-10 2022-10-20 Texas Tech University System Novel modified tetracyclines for treatment of alcohol use disorder, pain and other disorders involving potential inflammatory processes
AU2022215936A1 (en) 2021-02-03 2023-08-24 Consejo Nacional De Investigaciones Científicas Y Técnicas (Conicet) Chemically coupled transporter for low-hydrophobicity bioactive drugs into the central nervous system

Family Cites Families (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US21366A (en) 1858-08-31 Valve-cock
USRE26271E (en) * 1967-09-26 Reductive alkylation process
US2990331A (en) 1956-11-23 1961-06-27 Pfizer & Co C Stable solutions of salts of tetracyclines for parenteral administration
US2980584A (en) * 1957-10-29 1961-04-18 Pfizer & Co C Parenteral magnesium oxytetracycline acetic or lactic acid carboxamide vehicle preparation
US3062717A (en) 1958-12-11 1962-11-06 Pfizer & Co C Intramuscular calcium tetracycline acetic or lactic acid carboxamide vehicle preparation
US3043875A (en) * 1959-10-22 1962-07-10 Pfizer & Co C Halogenated tetracycline derivatives and processes for their preparation
FR1430859A (fr) * 1960-05-23 1966-05-25
US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3862225A (en) * 1961-08-18 1975-01-21 Pfizer D-ring substituted tetracyclines
US3165531A (en) 1962-03-08 1965-01-12 Pfizer & Co C 13-substituted-6-deoxytetracyclines and process utilizing the same
US3148212A (en) * 1961-12-22 1964-09-08 American Cyanamid Co Reductive alkylation process
USRE26253E (en) * 1963-05-17 1967-08-15 And z-alkylamino-g-deoxytetracycline
US3609188A (en) * 1964-10-29 1971-09-28 American Cyanamid Co 4-dedimethylamino-4-substituted-amino-6-demethyltetracyclines
US3454697A (en) * 1965-06-08 1969-07-08 American Cyanamid Co Tetracycline antibiotic compositions for oral use
US3304227A (en) 1965-07-15 1967-02-14 Loyal E Loveless Antibiotic-containing animal feed
US3433834A (en) * 1966-03-14 1969-03-18 American Cyanamid Co Nitration of 11a-chloro tetracyclines
US3397230A (en) * 1966-03-14 1968-08-13 American Cyanamid Co Nitration of tetracyclines
US3341585A (en) * 1966-05-06 1967-09-12 American Cyanamid Co Substituted 7-and/or 9-amino-6-deoxytetracyclines
NL6607516A (fr) 1966-05-31 1967-12-01
US3403179A (en) * 1967-01-10 1968-09-24 American Cyanamid Co Novel 7-(1, 2-bis-substituted-hydrazino)-tetracyclines and methods of preparing same
US3373196A (en) * 1967-03-21 1968-03-12 American Cyanamid Co 7-and/or 9-(lower alkyl) amino-5a, 6-anhydrotetracyclines
US3518306A (en) * 1968-02-19 1970-06-30 American Cyanamid Co 7- and/or 9-(n-nitrosoalkylamino)-6-demethyl-6-deoxytetracyclines
US3579579A (en) * 1968-04-18 1971-05-18 American Cyanamid Co Substituted 7- and/or 9-amino-6-demethyl-6-deoxytetracyclines
DE1767891C3 (de) 1968-06-28 1980-10-30 Pfizer Verfahren zur Herstellung von wäßrigen arzneilichen Lösungen für die parenterale, perorale und lokale Anwendung mit einem Gehalt an einem Tetracyclinderivat
US3795707A (en) * 1970-12-28 1974-03-05 Rachelle Labor Italia Spa Manufacture of alpha-6-deoxytetracyclines
NL158172B (nl) * 1972-09-18 1978-10-16 Farmaceutici Italia Werkwijze voor het bereiden van tetracyclinederivaten met een substituent op de 7-plaats.
US3957980A (en) 1972-10-26 1976-05-18 Pfizer Inc. Doxycycline parenteral compositions
GB1469384A (en) 1974-06-25 1977-04-06 Farmaceutici Italia Tetracyclines
DE2442829A1 (de) 1974-09-06 1976-03-18 Merck Patent Gmbh Tetracyclische verbindungen und verfahren zu ihrer herstellung
US4018889A (en) 1976-01-02 1977-04-19 Pfizer Inc. Oxytetracycline compositions
US4126680A (en) 1977-04-27 1978-11-21 Pfizer Inc. Tetracycline antibiotic compositions
US4925833A (en) 1983-12-29 1990-05-15 The Research Foundation Of State University Of New York Use of tetracycline to enhance bone protein synthesis and/or treatment of osteoporosis
USRE34656E (en) 1983-12-29 1994-07-05 The Research Foundation Of State University Of New York Use of tetracycline to enhance bone protein synthesis and/or treatment of bone deficiency
US4704383A (en) 1983-12-29 1987-11-03 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions possessing anti-collagenolytic properties and methods of preparing and using same
US4666897A (en) 1983-12-29 1987-05-19 Research Foundation Of State University Inhibition of mammalian collagenolytic enzymes by tetracyclines
US4935412A (en) 1983-12-29 1990-06-19 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions possessing anti-collagenolytic properties and methods of preparing and using same
US4946453A (en) * 1988-04-14 1990-08-07 Monson Demetrius A Weight reducing athletic garment
US5388391A (en) 1988-12-19 1995-02-14 Parker; Richard D. Apparatus and process for packaging biohazardous wastes
JP3016587B2 (ja) 1989-12-04 2000-03-06 ザ・リサーチ・ファンデーション・オブ・ステート・ユニバーシティ・オブ・ニューヨーク 非ステロイド抗炎症剤及びテトラサイクリンの配合
US5308839A (en) 1989-12-04 1994-05-03 The Research Foundation Of State University Of New York Composition comprising non-steroidal anti-inflammatory agent tenidap and effectively non-antibacterial tetracycline
US5770588A (en) 1991-02-11 1998-06-23 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions of the prevention and treatment of root caries
US5231017A (en) 1991-05-17 1993-07-27 Solvay Enzymes, Inc. Process for producing ethanol
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
US5281628A (en) * 1991-10-04 1994-01-25 American Cyanamid Company 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines
DE122006000058I1 (de) 1991-10-04 2007-01-18 Wyeth Corp 7-Substituierte-9-substituierte Amino-6-Demethyl-6-Deoxy-Tetracycline
US6756365B2 (en) * 1991-11-06 2004-06-29 Trustees Of Tufts College Reducing tetracycline resistance in living cells
US5258371A (en) 1992-05-29 1993-11-02 Kuraray Co., Ltd. Method to reduce connective tissue destruction
US6043225A (en) 1992-06-12 2000-03-28 Board Of Regents Of The University Of Washington Diagnosis and treatment of arterial chlamydial granuloma
US5284963A (en) 1992-08-13 1994-02-08 American Cyanamid Company Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
SG47520A1 (en) * 1992-08-13 1998-04-17 American Cyanamid Co New method for the production of 9-amino-6-demethyl-6-deoxytetracycline
US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5420272A (en) * 1992-08-13 1995-05-30 American Cyanamid Company 7-(substituted)-8-(substituted)-9-](substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5442059A (en) * 1992-08-13 1995-08-15 American Cyanamid Company 9-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracyclines
DK0599397T3 (da) 1992-11-17 1996-09-16 Univ New York State Res Found Tetracycliner, herunder non-mikrobielle, kemisk-modificerede tetracycliner, inhiberer overdreven collagentværbinding ved diabetes
US6043231A (en) 1993-03-02 2000-03-28 The Research Foundation Of State Univ. Of New York Inhibition of excessive phospholipase A2 activity and/or production by non-antimicrobial tetracyclines
US5523297A (en) * 1993-03-02 1996-06-04 The Research Foundation Of State University Of New York Inhibition of excessive phospholipase A2 activity and/or production by non-antimicrobial tetracyclines
US5371076A (en) * 1993-04-02 1994-12-06 American Cyanamid Company 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines
US5668122A (en) 1993-07-28 1997-09-16 Fife; Rose S. Method to treat cancer with tetracyclines
WO1995022529A1 (fr) 1994-02-17 1995-08-24 Pfizer Inc. Derives de 9-(amino-substitues)-alpha-6-deoxy-5-oxy tetracycline, leur preparation et leur utilisation comme antibiotiques
US5843925A (en) 1994-12-13 1998-12-01 American Cyanamid Company Methods for inhibiting angiogenesis, proliferation of endothelial or tumor cells and tumor growth
US5834449A (en) 1996-06-13 1998-11-10 The Research Foundation Of State University Of New York Treatment of aortic and vascular aneurysms with tetracycline compounds
US5827840A (en) 1996-08-01 1998-10-27 The Research Foundation Of State University Of New York Promotion of wound healing by chemically-modified tetracyclines
US5789395A (en) 1996-08-30 1998-08-04 The Research Foundation Of State University Of New York Method of using tetracycline compounds for inhibition of endogenous nitric oxide production
US5919774A (en) 1996-12-10 1999-07-06 Eli Lilly And Company Pyrroles as sPLA2 inhibitors
US5837696A (en) 1997-01-15 1998-11-17 The Research Foundation Of State University Of New York Method of inhibiting cancer growth
US5773430A (en) 1997-03-13 1998-06-30 Research Foundation Of State University Of New York Serine proteinase inhibitory activity by hydrophobic tetracycline
US6063775A (en) * 1997-04-29 2000-05-16 Berman; Charles L. Retardation of metalloproteinase incidental to HIV and/or AIDS
US5929055A (en) 1997-06-23 1999-07-27 The Research Foundation Of State University Of New York Therapeutic method for management of diabetes mellitus
JP2002501026A (ja) * 1998-01-23 2002-01-15 トルスティーズ オブ トゥフツ カレッジ 薬学的に活性の化合物及びその利用法
US6277061B1 (en) 1998-03-31 2001-08-21 The Research Foundation Of State University Of New York Method of inhibiting membrane-type matrix metalloproteinase
US6015804A (en) 1998-09-11 2000-01-18 The Research Foundation Of State University Of New York Method of using tetracycline compounds to enhance interleukin-10 production
US5977091A (en) 1998-09-21 1999-11-02 The Research Foundation Of State University Of New York Method of preventing acute lung injury
CA2343038A1 (fr) * 1998-09-28 2000-04-06 Maria Emanuel Ryan Nouvel inhibiteur de formation de cataracte
US5998390A (en) 1998-09-28 1999-12-07 The Research Foundation Of State University Of New York Combination of bisphosphonate and tetracycline
NZ511194A (en) 1998-11-18 2003-08-29 Collagenex Pharm Inc 4-dedimethylamino tetracycline derivatives
US6506740B1 (en) * 1998-11-18 2003-01-14 Robert A. Ashley 4-dedimethylaminotetracycline derivatives
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
DK1240133T3 (da) 1999-09-14 2006-08-21 Tufts College Fremgangsmåde til fremstilling af substituerede tetracycliner med overgangsmetalbaserede kemiske metoder
US6500812B2 (en) * 1999-09-14 2002-12-31 Paratek Pharmaceuticals, Inc. 13-substituted methacycline compounds
US6849615B2 (en) * 1999-09-14 2005-02-01 Paratek Pharmaceuticals, Inc. 13-substituted methacycline compounds
US6231894B1 (en) 1999-10-21 2001-05-15 Duke University Treatments based on discovery that nitric oxide synthase is a paraquat diaphorase
AU3105801A (en) * 2000-01-24 2001-07-31 Trustees Of Tufts College Tetracycline compounds for treatment of cryptosporidium parvum related disorders
AU2001281489A1 (en) * 2000-03-10 2001-10-03 Trustees Of Tufts College NIMR compositions and their methods of use
KR20030007489A (ko) * 2000-03-31 2003-01-23 트러스티즈 오브 터프츠 칼리지 7- 및 9-카르바메이트, 우레아, 티오우레아,티오카르바메이트 및 헤테로아릴-아미노 치환된테트라사이클린 화합물
DE60102815D1 (de) * 2000-05-15 2004-05-19 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
WO2001098259A1 (fr) 2000-06-16 2001-12-27 Trustees Of Tufts College Composes de tetracycline 7-phenyl-substituee
US20020132798A1 (en) * 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
AU2001268475A1 (en) * 2000-06-16 2002-01-02 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US20020128237A1 (en) * 2000-06-16 2002-09-12 Nelson Mark L. 7-N-substituted phenyl tetracycline compounds
US7094806B2 (en) * 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
CA2415086A1 (fr) * 2000-07-07 2002-01-17 Trustees Of Tufts College Composes de tetracycline substitues en 7, 8 et 9
US20050143353A1 (en) * 2000-07-07 2005-06-30 Paratek Pharmaceuticals, Inc. 13-Substituted methacycline compounds
BR0112265A (pt) * 2000-07-07 2003-06-24 Tufts College Compostos de tetraciclina substituìda, e de sanciclina 7-substituìda, método para tratar um estado responsivo à tetraciclina em um indivìduo, e, composição farmacêutica
SI1301467T1 (sl) * 2000-07-07 2007-02-28 Tufts College 9-substituirane minociklinske spojine
US7553828B2 (en) * 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
EP1241160A1 (fr) * 2001-03-13 2002-09-18 Glaxo Group Limited Dérivés de tétracyclines et leur utilisation comme agents antibiotiques
WO2002072506A2 (fr) * 2001-03-13 2002-09-19 Paratek Pharmaceuticals, Inc. Composes de 7-pyrollyl tetracycline et procedes d'utilisation associes
MXPA03008165A (es) * 2001-03-13 2003-12-12 Paratek Pharm Innc Compuestos tetraciclina sustituidos en la posicion 7,9.
US7045507B2 (en) * 2001-03-14 2006-05-16 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
WO2002072022A2 (fr) * 2001-03-14 2002-09-19 Paratek Pharmaceuticals, Inc. Composes de tetracycline substitues, en tant qu'agents antifongiques
EP1712236A3 (fr) * 2001-04-05 2008-05-28 Collagenex Pharmaceuticals, Inc. Dérivés du tetracycline destinés au traitement de l'acné
ES2338994T3 (es) * 2001-04-24 2010-05-14 Paratek Pharmaceuticals, Inc. Compuestos de tetraciclina sustituida para el tratamiento de la malaria.
EP1408987B1 (fr) * 2001-07-13 2013-04-10 Paratek Pharmaceuticals, Inc. Composes de tetracycline a activites therapeutiques cibles
WO2003056294A2 (fr) * 2001-07-13 2003-07-10 Paratek Pharmaceuticals, Inc. Methodes d'identification et d'utilisation de composes de liaison de polypeptides de la famille marr
US20060194773A1 (en) * 2001-07-13 2006-08-31 Paratek Pharmaceuticals, Inc. Tetracyline compounds having target therapeutic activities
MY133403A (en) * 2001-10-05 2007-11-30 Tetragenex Pharmaceuticals Inc Tetracycline derivatives and methods of use thereof
AU2003235759A1 (en) * 2002-01-08 2003-07-24 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
KR101163937B1 (ko) * 2002-03-08 2012-07-09 파라테크 파마슈티컬스, 인크. 아미노-메틸 치환된 테트라시클린 화합물
EP1503981A4 (fr) * 2002-03-21 2007-08-15 Paratek Pharm Innc Derives substitues de tetracycline
US7553827B2 (en) * 2003-08-13 2009-06-30 Depuy Spine, Inc. Transdiscal administration of cycline compounds
WO2005009943A2 (fr) * 2003-07-09 2005-02-03 Paratek Pharmaceuticals, Inc. Composes de tetracycline substitues
JP4738333B2 (ja) * 2003-07-09 2011-08-03 パラテック ファーマシューティカルズ インコーポレイテッド ９−アミノメチルテトラサイクリン化合物のプロドラッグ
EP2332904A3 (fr) * 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derives des composes de tetracycline
US7858601B2 (en) * 2004-10-25 2010-12-28 Paratek Pharmaceuticals, Inc. 4-substituted tetracyclines and methods of use thereof
EP2284164A3 (fr) * 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Composés de tétracycline substituée
US20070093455A1 (en) * 2005-07-21 2007-04-26 Paul Abato 10-substituted tetracyclines and methods of use thereof

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005526754A (ja) * 2002-03-08 2005-09-08 パラテック ファーマシューティカルズ インコーポレイテッド アミノメチル置換されたテトラサイクリン化合物
JP2008266330A (ja) * 2002-03-08 2008-11-06 Paratek Pharmaceuticals Inc アミノメチル置換されたテトラサイクリン化合物
JP2005520846A (ja) * 2002-03-21 2005-07-14 パラテック ファーマシューティカルズ インコーポレイテッド 置換されたテトラサイクリン化合物。
JP2010513527A (ja) * 2006-12-21 2010-04-30 パラテック ファーマシューティカルズ インコーポレイテッド 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体
JP2014167027A (ja) * 2006-12-21 2014-09-11 Paratek Pharmaceuticals Inc 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体
JP2015205939A (ja) * 2006-12-21 2015-11-19 パラテック ファーマシューティカルズ インコーポレイテッド 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体
JP2018039846A (ja) * 2006-12-21 2018-03-15 パラテック ファーマシューティカルズ インコーポレイテッド 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体
JP2021063137A (ja) * 2006-12-21 2021-04-22 パラテック ファーマシューティカルズ，インコーポレイテッド 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体

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AU2003235759A8 (en) 2003-07-24
EP2322501B1 (fr) 2015-08-05
EP2311798A1 (fr) 2011-04-20
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US7056902B2 (en) 2006-06-06
US20060089336A1 (en) 2006-04-27
JP2010111690A (ja) 2010-05-20
US20160324880A1 (en) 2016-11-10
JP2015063557A (ja) 2015-04-09
AU2003235759A1 (en) 2003-07-24
JP2017178962A (ja) 2017-10-05
EP2311799A1 (fr) 2011-04-20
ES2551708T3 (es) 2015-11-23
EP1474380A2 (fr) 2004-11-10
EP2311797A1 (fr) 2011-04-20
EP2995610A1 (fr) 2016-03-16
EP2311796A1 (fr) 2011-04-20
US20040157806A1 (en) 2004-08-12
US9278911B2 (en) 2016-03-08

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